New Advances in Chemical Research, April 2021. Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. 4330-21-6, Name is Hoffer’s chlorosugar, SMILES is O=C(O[C@@H]1[C@@H](COC(C2=CC=C(C)C=C2)=O)O[C@H](Cl)C1)C3=CC=C(C)C=C3, belongs to dioxole compound. In a document, author is Lafite, Pierre, introduce the new discover, Recommanded Product: 4330-21-6.
Selective, competitive and mechanism-based inhibitors of human cytochrome P450 2J2
Twenty five derivatives of the drugs terfenadine and ebastine have been designed, synthesized and evaluated as inhibitors of recombinant human CYP2J2. Compound 14, which has an imidazole substituent, is a good non-competitive inhibitor of CYP2.12 (IC50 – 400 nM). It is not selective towards CYP2.12 as it also efficiently inhibits the other main vascular CYPs, such as CYP2B6, 2C8. 2C9 and 3A4: however, it could be an interesting tool to inhibit all these vascular CYPs. Compounds 4, 5 and 13, which have a propyl, allyl and benzo-1,3-dioxole terminal group, respectively, are selective CYP2J2 inhibitors. Compound 4 is a high-affinity, competitive inhibitor and alternative substrate of CYP2J2 (K-i = 160 50 nM). Compounds 5 and 13 are efficient mechanism-based inhibitors of CYP2J2 (k(inact)/K-i values similar to 3000 L mol(-1) s(-1)). Inactivation of CYP2J2 by 13 is due to the formation of a stable iron-carbene bond which occurs upon CYP2J2-catalyzed oxidation of 13 with a partition ratio of 18 +/- 3. These new selective inhibitors should be interesting tools to study the biological roles of CYP2J2. Published by Elsevier Inc.
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Reference:
1,3-Benzodioxole – Wikipedia,
,Dioxole | C3H4O2 – PubChem